AbstractIn southern California, the current method of choice for the synthesis of illicit methamphetamine is the reduction of ephedrine or pseudoephedrine with hydriodic acid and red phosphorus. However, as a result of restrictions on the availability of both precursors, common cold tablet preparations are increasingly being used as a source of ephedrine and pseudoephedrine. Such tablets also contain other ingredients such as paracetamol, chlorpheniramine, dextromethorphan, diphenhydramine, doxylamine, guaifenesin, and triprolidine. Depending on the isolation method used, these other compounds may be present in the reaction mixtures and subsequently produce other by-products. This paper describes the by-products formed as a result of the reaction between the tablet ingredients and hydriodic acid/red phosphorus. The identification of the by-products found in clandestine methamphetamine laboratories would help to determine the exact cold preparation used as the source of the precursor.____ ___ __ _

AbstractPrevious studies on the khat plant (Catha edulis) illustrated the importance of using freshly harvested young shoots and leaves such that cathinone, the principal active component and Schedule I controlled drug contained within the plant, could be suitably isolated and identified. Upon drying and storage of the cut plant material, cathinone readily converts to the reduced product, cathine, which necessitates rapid extraction and chemical analysis for cathinone identification. This study demonstrates that by air drying the young khat shoots at ambient temperature, cathinone may be detected in khat samples that have been harvested for more than 10 days. Refrigeration for two weeks and freezing for one month of the khat samples also yield identifiable levels of cathinone. Cathinone and cathine are both specifically determined and differentiated by vapor phase infrared detection, which is the method of choice in relation to mass spectrometry.____ ___ __ _

AbstractMass spectrometric data are presented for the detection of metabolites of the amphetamine derivates 3,4-(Methylenedioxy)amphetamine (MDA) und 3,4-(Methylenedioxy)methylamphetamine (MDMA, Ecstasy) as well as some other derivatives.____ ___ __ _

Intermediates/byproducts in the illegal production of fentanyl, and its p-fluoro- and N-acetyl analoguesFritschi G, Klein B.Arch Kriminol. 196(5-6), 149-55 (1995) [Article in German]

AbstractThe aim of the present work was the gaschromatographic and mass spectrometric characterization of intermediates and artifacts in the illegal synthesis of fentanyl and fluorfentanyls. These data provide the means to recognize fentanyls from illicit production.____ ___ __ _

Fentanyl analogues with a modified propanamido group as potential affinity labels: synthesis and in vivo activity.Essawi MYH.Pharmazie 54(4), 307–8 (1999)

AbstractA two-phase mixture (sodium bromide, aqueous hydrogen peroxide/carbon tetrachloride or chloroform) under visible light provides a simple and convenient system for benzylic bromination of toluenes. A high atomic yield for bromine atoms is attained. Substitution of the chlorinated solvents by other more environmentally benign organic solvents has been attempted and good results are obtained for methyl pivalate.

AbstractHydrazine aided catalytic transfer hydrogenation has been employed for the reduction of both aliphatic and aromatic nitro compounds to corresponding amines. The use of low-cost magnesium, as catalyst leads to high yields of amino compounds under ambient conditions of temperature and pressure. Many commonly encountered functional groups like ethene, nitrile, acid, phenol, halogen etc. are compatible with the present system.____ ___ __ _

AbstractThe reduction of nitro compounds, both aliphatic and aromatic into corresponding amines has been achieved at room temperature in good yields by employing ammonium formate in the presence of low cost magnesium powder. The hydrogenation is fast and selective in the presence of other sensitive functionalities such as halogens, -OH, -OCH3, -CN, -COOR, -COOH etc. It was observed that, this system is equally compatible with existing methods, which employ expensive catalysts like palladium, platinum, ruthenium etc.

AbstractChromite catalysts have been studied with and without modifiers for lactonization of 1,4-butanediol. The reaction on majority of the catalyst proceeds giving rise to cyclodehydration product, tetrahydrofuran (THF) mainly rather than cyclodehydrogenation product of gamma-butyrolactone (gamma-BL). The lactonization of 1,4-butanediol increases when the zinc chromite catalyst is modified with Pt metal. Few methods are discussed regarding the preparation and modification of the catalysts and their effects in selectivity from THF to gamma-BL.

AbstractA review of the most important synthetic approaches to cocaine and its analogs with 95 refs. It is presented in the following chapters; (1) Introduction (2) Total synthesis of cocaine via Mannich-type cyclization, nitrone-based approach, and Dieckmann cyclization (3) Synthesis of anhydroecgonine methylester (4) Synthesis of cocaine's analogs (5) Conclusions. Particular attention has been devoted to the recent synthetic acquisitions esp. regarding the synthesis of two-carbon bridge substituted cocaines as well as to conformationally restricted cocaine derivs.(Please scan the pages in an OCR-friendly way, as in completely straight and in 200 DPI. Do not compress with jpg/djvu.)

AbstractPhCH2Cl was prepd. by chlorination of PhMe with Ca(OCl)2 using tetrabutylammonium hydrogen sulfate or tetrabutylammonium bromide as phase-transfer catalysts. With suitable ratio of PhMe-catalyst, the yield was high and the reaction was quite selective.____ ___ __ _

The synth for this powerful opiate is very straightforward except for the difficulty in obtaining 2-(1,4-Cyclohexadienyl)ethylamine. This compound can be made from PEA (decarboxylate phenylalanine) with a controlled birch reduction of the ring, however the reference given here would seem to procede from cyclohexanone or cyclohexanol which would offer a far simpler route.

AbstractDextrorphan is the main metabolite of Dextromethorphan, a drug with high anti-tussive activity.In this preliminary work we report on the synthesis of two essential intermediates for its preparation: 2-(1-cyclohexenyl)ethyl amine and (R;S)-1-(4-methoxy-benzyl)-2-methyl-1,2,3,4,5,6,7,8-octahydroisoquinoline.

AbstractSalvinorin A (1), a nonnitrogenous, neoclarodane diterpine, obtained from Salvia divinorum, has been reported to be the most potent naturally occurring hallucinogen, with an ED in humans in the 200- to 1,000- micrograms range when smoked with a typical duration of action being several minutes to an hour. Salvia divinorum exts. and salvinorin A have become widely used in the U.S. as legal hallucinogens. The site of pharmacol. activity remained a mystery until the recent report that identified salvinorin A as a potent and selective ligand for the kappa-opioid receptor. Thus representing a unique structural class of nonnitrogenous opioid ligands. In order to investigate structure-activity relationships of salvinorin A, analogs must be made. One approach to analog synthesis is from a total synthesis perspective. To our knowledge, there are no known syntheses of salvinorin A. Here we report our progress toward the first total synthesis of salvinorin A.

Some years ago a report appeared in the forensic literature of Italy, of the seizure of a small semitransparent capsule containing 141 milligrams of a white powder that was stated to be a new hallucinogenic drug. This was shown to contain an analogue of DOM, 3-methoxy-4-methylamphetamine, or MMA. The Italian authorities made no mention of the net weight contained in each dosage unit, but it has been found that the active level of MMA in man is in the area of 40-60 milligrams. The compound can apparently be quite dysphoric, and long lived.

There are several questions that may be answered in this article:1) Are there anecdotal reports on the effects of MMA in humans?2) How was the structure of the seized substance elucidated? Is there any possibility that it could be actually an isomer of MMA, say, 4-MeO-3-Me-A, PMMA, or 4-MeO-3,5-diMe-PEA?3) What method was applied to synthesize the substance?

AbstractReimer-Tiemann reaction and a methoxylation through di-Me sulfate are employed for the prepn. of 2,5-dimethoxybenzaldehyde from p-methoxyphenol in this paper. Comparing different phase transfer catalysts, it can be demonstrated that the PEG-10000 is the most favorable catalyst used in Reimer-Tiemann reaction. The yield and quality are improved through the methoxylation of 2-hydroxy-5-methoxy-benzaldehyde in a buffer soln. The diverse factors influencing the yield are examd. Some explanations are given from theor. viewpoint. The proper exptl. conditions are found and the overall yield reached 68%.____ ___ __ _

AbstractThe compn. of the Z. cassumunar oil from Indonesia was examd. by gas chromatog. (GC) and GC-mass spectrometry. A major part of the oil consists of monoterpenes with sabinene and terpinen-4-ol as main constituents. Sesquiterpenes accounted for a small part of the oil with sesquiphellandrene being the principal constituent. In addn. to these terpenes the oil contains a no. of phenylbutanoids. The essential oil obtained by steam contained about 25% of these phenylbutanoids whereas, the oil obtained by extn. with light petroleum had about 46% with trans-1-(3,4-dimethoxyphenyl)but-1-ene, trans-1-(3,4-dimethoxyphenyl)butadiene and trans-4-(3,4-dimethoxyphenyl)but-3-ene-1-yl acetate as the main constituents.

josef_k

Could someone get these articles drone mentioned on the reaction of the quaternary N-methyl-4-piperidone methiodide with amines to get N-substituted 4-piperidones.

Chem. Heterocycl. Compd. 21(12) 1327

Also, in an article I saw they alkylated 4-piperidone pyrrolidine enamine with allylbromide to get 3-allyl-4-piperidone but they didn't give reaction details or references. That kind of reaction would be useful for making 3-methyl piperidones.

Chem. Heterocycl. Compd. 21(12): 1362

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Vitus_Verdegast

Here is something interesting in the pursuit of AMT from isatin:3-Methyleneoxindoles can be selectively reduced at the carbon-carbon double bond using sodium dithionite in aqueous ethanol.Isatylideneacetones are reduced to the corresponding 3-acetonyloxindoles in 57-92% yield.

(Nicodem: "Modifications on the side chain (again)", Novel Discourse) :

“The alpha-methyl group of amphetamine itself can be replaced by allyl, ethyl, or ethynyl groups of electron-donating character, without deleterious effects on centrally-mediated actions [1,2], but replacement by electron-withdrawing groups, such as cyano [3] or trifluoromethyl [4], abolishes amphetamine-like properties.”

If anybody can find and post them, these are the refs for the phenoxyethylamines:Julia, M. and de Rosnay; European Journal of Medicinal Chemistry, 4 (1969), 334.Julia, M. and de Rosnay; European Journal of Medicinal Chemistry, 5 (1970), 337.(European J. of Med. Chem. stil had the title Chim. Ther. in those times)Rougeul, A.; Laval. med., 40 (1969), 37.Rougeul, A. and Verdaux, J.; Rev. Can. Biol., 31 (1972), 49.

AbstractAlthough gamma-butyrolactone (GBL) rapidly converts to gamma-hydroxybutyrate (GHB) in vivo, the lactone gave significantly more prolonged hypnotic effects than GHB when equimolar doses were compared both parenterally and orally in rats. Plasma drug concentrations were higher after GBL administration through both routes, consistent with the observed differences in the pharmacological activity of these two compounds. Oral GBL was absorbed much faster than oral GHB, with the dual effects of decreasing potential first-pass metabolism and elevating plasma drug concentrations to the region where capacity-limited elimination is operative. Parenteral GBL produced a slower initial drug plasma clearance than parenteral GHB. In spite of the rapid metabolism of GBL to GHB, the apparent tissue distribution of these two compounds may be different.

AbstractFe2+ halide or Feo-Fe3+ system as a promoter for the Sandmeyer reaction, wherein Cu+ causes detrimental side effects in the case of Me-substituted or ortho-substituted arenediazonium salts, was discussed. The oxidn. of pendant Me groups was not evident in the Fe system and the reaction was applicable to a wide variety of functional groups. The Fe system is less expensive than Cu+ and more friendly environmentally.

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Disciple

HiI've hada bit of a fish aroundlooking for this but haven't found anything yet if someones got access to this thanks.Physical characterization of the new bis(N-phenylpiperazines). Journal of Pharmacy (University of Karachi) (1985), 3(2), 89-94.

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Stalin

I would be interested in the following two articles, especially because of their historical context:

The Drug Problem in the Military: an American Lawyer's Point of View. Medicine, Science and the Law 9(2) (1969) 122-124Hallucinogens and Narcotics Alarm Public. Chemical and Engineering News 48(47) (1970) 44-45